WO2009027346A3 - Inhibiteurs 17bêta-hydroxystéroïd-déhydrogénase de type 1 pour traiter des maladies hormono-dépendantes - Google Patents

Inhibiteurs 17bêta-hydroxystéroïd-déhydrogénase de type 1 pour traiter des maladies hormono-dépendantes Download PDF

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Publication number
WO2009027346A3
WO2009027346A3 PCT/EP2008/061033 EP2008061033W WO2009027346A3 WO 2009027346 A3 WO2009027346 A3 WO 2009027346A3 EP 2008061033 W EP2008061033 W EP 2008061033W WO 2009027346 A3 WO2009027346 A3 WO 2009027346A3
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WO
WIPO (PCT)
Prior art keywords
17beta
inhibitors
hormone
treatment
hydroxysteroid dehydrogenase
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PCT/EP2008/061033
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German (de)
English (en)
Other versions
WO2009027346A2 (fr
Inventor
Rolf Hartmann
Martin Frotscher
Sandrine Oberwinkler
Emmanuel Bey
Original Assignee
Univ Saarland
Rolf Hartmann
Martin Frotscher
Sandrine Oberwinkler
Emmanuel Bey
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Publication date
Application filed by Univ Saarland, Rolf Hartmann, Martin Frotscher, Sandrine Oberwinkler, Emmanuel Bey filed Critical Univ Saarland
Priority to EP08787432A priority Critical patent/EP2190421A2/fr
Priority to US12/675,065 priority patent/US20110046147A1/en
Priority to CA2697827A priority patent/CA2697827A1/fr
Priority to JP2010522332A priority patent/JP2010536922A/ja
Publication of WO2009027346A2 publication Critical patent/WO2009027346A2/fr
Publication of WO2009027346A3 publication Critical patent/WO2009027346A3/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/39—Heterocyclic compounds having sulfur as a ring hetero atom having oxygen in the same ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A—HUMAN NECESSITIES
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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    • C07—ORGANIC CHEMISTRY
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    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
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    • C07—ORGANIC CHEMISTRY
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    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
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    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms

Abstract

L'invention concerne des inhibiteurs 17bêta-hydroxystéroïd-déhydrogénase de type 1 (17bêtaHSD1), leur production et leur utilisation pour le traitement prophylactique et thérapeutique de maladies hormono-dépendantes, notamment de maladies dépendant d'oestrogènes ou d'androgènes.
PCT/EP2008/061033 2007-08-25 2008-08-22 Inhibiteurs 17bêta-hydroxystéroïd-déhydrogénase de type 1 pour traiter des maladies hormono-dépendantes WO2009027346A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP08787432A EP2190421A2 (fr) 2007-08-25 2008-08-22 Inhibiteurs 17bêta-hydroxystéroïd-déhydrogénase de type 1 pour traiter des maladies hormono-dépendantes
US12/675,065 US20110046147A1 (en) 2007-08-25 2008-08-22 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
CA2697827A CA2697827A1 (fr) 2007-08-25 2008-08-22 Inhibiteurs 17beta-hydroxysteroid-dehydrogenase de type 1 pour traiter des maladies hormono-dependantes
JP2010522332A JP2010536922A (ja) 2007-08-25 2008-08-22 ホルモン関連疾患治療用の１７ベータ−ヒドロキシステロイドデヒドロゲナーゼ１型阻害剤

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102007040243A DE102007040243A1 (de) 2007-08-25 2007-08-25 17Beta-Hydroxysteriod-Dehydrogenase Typ1 Inhibitoren zur Behandlung hormonabhängiger Erkrankungen
DE102007040243.2 2007-08-25

Publications (2)

Publication Number Publication Date
WO2009027346A2 WO2009027346A2 (fr) 2009-03-05
WO2009027346A3 true WO2009027346A3 (fr) 2009-05-28

Family

ID=39929888

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2008/061033 WO2009027346A2 (fr) 2007-08-25 2008-08-22 Inhibiteurs 17bêta-hydroxystéroïd-déhydrogénase de type 1 pour traiter des maladies hormono-dépendantes

Country Status (6)

Country Link
US (1) US20110046147A1 (fr)
EP (1) EP2190421A2 (fr)
JP (1) JP2010536922A (fr)
CA (1) CA2697827A1 (fr)
DE (1) DE102007040243A1 (fr)
WO (1) WO2009027346A2 (fr)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9187485B2 (en) 2007-02-02 2015-11-17 Baylor College Of Medicine Methods and compositions for the treatment of cancer and related hyperproliferative disorders
KR101675175B1 (ko) * 2009-02-19 2016-11-10 메르크 파텐트 게엠베하 티오펜 유도체 및 이를 함유하는 액정 매질
US8865754B2 (en) 2011-03-03 2014-10-21 Proteotech Inc. Compounds for the treatment of neurodegenerative diseases
ES2489815B1 (es) * 2013-02-21 2015-08-10 Centro De Investigación Príncipe Felipe Nuevos p-terfenilos hexakis-sustituidos con grupos bilaterales para el tratamiento de la infección por el virus de la inmunodeficiencia humana tipo 1 (VIH-1) y otras enfermedades
WO2015031710A1 (fr) * 2013-08-29 2015-03-05 Baylor College Of Medicine Compositions et procédés de traitement de troubles métaboliques et troubles associés au poids corporel
US9884839B2 (en) 2014-01-03 2018-02-06 Elexopharm Gmbh Inhibitors of 17Beta-hydroxysteroid dehydrogenases type 1 and type 2
KR20160115999A (ko) 2014-02-14 2016-10-06 더 유니버시티 오브 브리티쉬 콜롬비아 치료제로서의 인간 안드로겐 수용체 dna-결합 도메인(dbd) 화합물 및 그의 사용 방법
WO2015166862A1 (fr) * 2014-04-30 2015-11-05 日本カーバイド工業株式会社 Procede de production d'un compose de bispyrazole
US10328064B2 (en) 2014-12-23 2019-06-25 Fgh Biotech, Inc. Compositions of fatostatin based heterocyclic compounds and uses thereof
KR102655928B1 (ko) * 2015-06-23 2024-04-09 깃세이 야쿠힌 고교 가부시키가이샤 피라졸 유도체, 또는 그 약리학적으로 허용되는 염
CN105348218A (zh) * 2015-12-08 2016-02-24 彭冬青 一种治疗慢性子宫内膜炎的药物组合物
SG11201804901WA (en) * 2015-12-22 2018-07-30 SHY Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
ES2912921T3 (es) 2016-04-29 2022-05-30 Fgh Biotech Inc Compuestos de pirazol disustituidos para el tratamiento de enfermedades
EP3510027B1 (fr) 2016-09-07 2022-11-02 FGH BioTech, Inc. Composés de pyrazole di-substitués pour le traitement de maladies
EA201992780A1 (ru) 2017-06-21 2020-06-02 ШАЙ ТЕРАПЬЮТИКС ЭлЭлСи Соединения, которые взаимодействуют с суперсемейством ras, для лечения рака, воспалительных заболеваний, ras-опатий и фиброзного заболевания
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
WO2021211981A1 (fr) * 2020-04-18 2021-10-21 Inipharm, Inc. Inhibiteurs de hsd17b13 sélectifs d'un substrat et utilisations de ceux-ci
EP4291307A1 (fr) * 2021-02-09 2023-12-20 Oregon State University Dérivés de xanthohumol et procédés de fabrication et méthodes d'utilisation associés

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1970656A (en) * 1931-11-04 1934-08-21 Winthrop Chem Co Inc Thiazole compound and process of producing the same
WO2000008001A1 (fr) * 1998-08-07 2000-02-17 Chiron Corporation Isoxazoles substitues comme modulateurs de recepteur d'oestrogenes
WO2000019994A1 (fr) * 1998-10-02 2000-04-13 Board Of Trustees Of The University Of Illinois Ligands se liant aux recepteurs d'oestrogenes
WO2004000820A2 (fr) * 2002-06-21 2003-12-31 Cellular Genomics, Inc. Monocycles aromatiques utilises comme modulateurs de la kinase
EP1398029A1 (fr) * 2002-09-10 2004-03-17 LION Bioscience AG Derivés de pyrazole,substitués en position 3 ayant une affinité envers le NR3B1 récepteur
WO2006022955A2 (fr) * 2004-05-27 2006-03-02 Propharmacon, Inc. Inhibiteurs de topoisomerase
WO2006044975A2 (fr) * 2004-10-19 2006-04-27 Compass Pharmaceuticals Llc Compositions et leur utilisation comme agents antitumoraux
EP1685150A2 (fr) * 2003-11-12 2006-08-02 Solvay Pharmaceuticals GmbH NOUVEAUS INHIBITORS DE 17beta HYDROXYSTEROID DEHYDROGENASE TYPE I
WO2006092059A1 (fr) * 2005-03-04 2006-09-08 Fan Wu Conception et synthese de nouvelles substances antimicrobiennes
WO2006109680A1 (fr) * 2005-04-07 2006-10-19 Nippon Kayaku Kabushiki Kaisha Utilisation d'un analogue du 3,5-diphenylpyrazole en tant qu'agent antitumoral
US20070197832A1 (en) * 2006-02-07 2007-08-23 Azuma Rie Method of producing poly(ortho-methylphenol)

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH03251494A (ja) * 1990-03-01 1991-11-08 Oji Paper Co Ltd 感熱記録体
WO2003000249A1 (fr) * 2001-06-26 2003-01-03 Takeda Chemical Industries, Ltd. Regulateur de la fonction du recepteur relatif aux retinoides
WO2004080972A1 (fr) * 2003-03-12 2004-09-23 Vertex Pharmaceuticals Incorporated Pyrazoles, modulateurs de transporteurs de cassettes de liaison a l'atp
US7754709B2 (en) 2003-06-10 2010-07-13 Solvay Pharmaceuticals Bv Tetracyclic thiophenepyrimidinone compounds as inhibitors of 17β hydroxysteroid dehydrogenase compounds
US7465739B2 (en) 2003-06-10 2008-12-16 Solvay Pharmaceuticals B.V. Compounds and their use in therapy
US20050228038A1 (en) 2004-04-08 2005-10-13 Vander Jagt David L 11-Beta hydroxysteroid dehydrogenase type 1 inhibitors as anti-obesity/anti-diabetes compounds and 17-beta hydrosteroid dehydrogenase type I inhibitors as useful agents for the treatment of cancers, especially breast cancer
DE102004032673A1 (de) 2004-07-02 2006-01-26 Schering Ag Neue 2-substituierte D-Homo-estra-1,3,5(10)-triene als Inhibitoren der 17ß-Hydroxysteroiddehydrogenase Typ 1
US7435757B2 (en) 2004-07-02 2008-10-14 Schering Ag 2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17β-hydroxy steroid dehydrogenase type 1

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1970656A (en) * 1931-11-04 1934-08-21 Winthrop Chem Co Inc Thiazole compound and process of producing the same
WO2000008001A1 (fr) * 1998-08-07 2000-02-17 Chiron Corporation Isoxazoles substitues comme modulateurs de recepteur d'oestrogenes
WO2000019994A1 (fr) * 1998-10-02 2000-04-13 Board Of Trustees Of The University Of Illinois Ligands se liant aux recepteurs d'oestrogenes
WO2004000820A2 (fr) * 2002-06-21 2003-12-31 Cellular Genomics, Inc. Monocycles aromatiques utilises comme modulateurs de la kinase
EP1398029A1 (fr) * 2002-09-10 2004-03-17 LION Bioscience AG Derivés de pyrazole,substitués en position 3 ayant une affinité envers le NR3B1 récepteur
EP1685150A2 (fr) * 2003-11-12 2006-08-02 Solvay Pharmaceuticals GmbH NOUVEAUS INHIBITORS DE 17beta HYDROXYSTEROID DEHYDROGENASE TYPE I
WO2006022955A2 (fr) * 2004-05-27 2006-03-02 Propharmacon, Inc. Inhibiteurs de topoisomerase
WO2006044975A2 (fr) * 2004-10-19 2006-04-27 Compass Pharmaceuticals Llc Compositions et leur utilisation comme agents antitumoraux
WO2006092059A1 (fr) * 2005-03-04 2006-09-08 Fan Wu Conception et synthese de nouvelles substances antimicrobiennes
WO2006109680A1 (fr) * 2005-04-07 2006-10-19 Nippon Kayaku Kabushiki Kaisha Utilisation d'un analogue du 3,5-diphenylpyrazole en tant qu'agent antitumoral
US20070197832A1 (en) * 2006-02-07 2007-08-23 Azuma Rie Method of producing poly(ortho-methylphenol)

Non-Patent Citations (11)

* Cited by examiner, † Cited by third party
Title
BALCAR: "Reaktivität von Stickstoff-Heterocyclen gegenüber Cyclooctin als Dienophil", TETRAHEDRON LETTERS, vol. 24, no. 14, 1 January 1983 (1983-01-01), pages 1481 - 1484, XP007906413 *
BENTISS F; LAGRENEE M: "A new synthesis of symmetrical 2,5-disubstituted 1,3,4- oxadiazoles", JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 36, no. 4, 1 January 1999 (1999-01-01), pages 1029 - 1032, XP009108808 *
BEY EMMANUEL ET AL: "Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17 beta-hydroxysteroid dehydrogenase type 1 (17 beta-HSD1) for the treatment of estrogen-dependent diseases", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 16, no. 12, June 2008 (2008-06-01), pages 6423 - 6435, XP002504624, ISSN: 0968-0896 *
CHALK: "A new pyridine synthesis from conjugated acetylenes and substituted methylamines", TETRAHEDRON, vol. 30, 1 January 1974 (1974-01-01), pages 1387 - 1391, XP007906414 *
FINK B E ET AL: "NOVEL STRUCTURAL TEMPLATES FOR ESTROGEN-RECEPTOR LIGANDS AND PROSPECTS FOR COMBINATORIAL SYNTHESIS OF ESTROGENS", CHEMISTRY AND BIOLOGY, CURRENT BIOLOGY, LONDON, GB, vol. 6, no. 4, 1 January 1999 (1999-01-01), pages 205 - 219, XP000905542, ISSN: 1074-5521 *
KOROTKIKH N I ET AL: "SYNTHESIS OF 1,3,4-OXIDIAZOLE AND XANTHEN-2-ONE LUMINOPHORIC EPOXIDE MONOMERS", CHEMISTRY OF HETEROCYCLIC COMPOUNDS (A TRANSLATION OF KHIMIYAGETEROTSIKLICHESKIKH SOEDINENII), PLENUM PRESS CO., NEW YORK, NY, US, vol. 35, no. 3, 1 January 1999 (1999-01-01), pages 358 - 362, XP008024157, ISSN: 0009-3122 *
KRIEG B ET AL: "UEBER EINIGE NEUE IMIDAZOLDERIVATE", CHEMISCHE BERICHTE, VERLAG CHEMIE GMBH. WEINHEIM, DE, vol. 100, no. 12, 1 January 1967 (1967-01-01), pages 4042 - 4049, XP009059651, ISSN: 0009-2940 *
LEBRINI M ET AL: "Rapid synthesis of 2,5-disubtituted 1,3,4-thiadiazoles under microwave irradiation", JOURNAL OF HETEROCYCLIC CHEMISTRY, HETEROCORPORATION. PROVO, US, vol. 42, no. 5, 1 July 2005 (2005-07-01), pages 991 - 994, XP009108658, ISSN: 0022-152X *
PIRALI TRACEY ET AL: "Estrogenic analogues synthesized by click chemistry.", CHEMMEDCHEM APR 2007, vol. 2, no. 4, April 2007 (2007-04-01), pages 437 - 440, XP002504621, ISSN: 1860-7187 *
RAO G -W ET AL: "Synthesis, structure analysis, and antitumor activity of 3,6-disubstituted-1,4-dihydro-1,2,4,5-tetrazine derivatives", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS 20060715 GB, vol. 16, no. 14, 15 July 2006 (2006-07-15), pages 3702 - 3705, XP002504623, ISSN: 0960-894X *
SIMONI D ET AL: "Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines", JOURNAL OF MEDICINAL CHEMISTRY 20050210 US, vol. 48, no. 3, 10 February 2005 (2005-02-10), pages 723 - 736, XP002504622, ISSN: 0022-2623 *

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